Catalog No.S1658 Synonyms: UK-68798
Molecular Weight(MW): 441.56
Dofetilide is a selective potassium channel ((hERG)) blocker, used as a Class III antiarrhythmic drug.
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Choose Selective Potassium Channel Inhibitors
|Description||Dofetilide is a selective potassium channel ((hERG)) blocker, used as a Class III antiarrhythmic drug.|
Dofetilide blocks HERG currents in excised macro patches of Xenopus oocytes.  Dofetilide (1 μM) reduces the amplitude of IKr to 61% of control currents in guinea pig cardiomyocytes, as measured by 200-ms test pulses and analysis of the deactivating tail currents of IKr.  Dofetilide increases apico-basal disparity of repolarization, due to a more marked increase of ERPs in the apex than in the base in the intact canine heart. 
|In vivo||Dofetilide (100 mg/kg, i.v.) does not suppress automaticity arrhythmias induced by two-stage coronary ligation and epinephrine or the coronary ligation and reperfusion arrhythmias, but suppresses the reentry arrhythmia induced by PES in dogs with old myocardial infarction (MI). Dofetilide also shows antiarrhythmic effect in some dogs with digitalis arrhythmia. Dofetilide increases QT interval and shows negative chronotropic effect like that of other class III drugs, but is different in antiarrhythmic profiles from those of other class III agents such as D-sotalol, E-4031, and MS-551 in that it does not prevent the occurrence of ventricular fibrillation (VF) immediately after coronary reperfusion and has some antiarrhythmic effects on digitalis arrhythmia.  Dofetilide causes increased resorptions and the same stage-dependent malformations in Sprague-Dawley rats. |
-  Kiehn J, et al. Circulation, 1996, 94(10), 2572-2579.
-  Kiehn J, et al. J Cardiovasc Pharmacol, 1994, 24(4), 566-572.
-  Bauer A, et al. J Cardiovasc Pharmacol, 2002, 39(3), 460-467.
|In vitro||DMSO||88 mg/mL warmed (199.29 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02365532||Completed||Long QT Syndrome||Gilead Sciences||February 2015||Phase 1|
|NCT02308748||Completed||Drug-induced QT Prolongation|Pharmacokinetics|Pharmacodynamics||Food and Drug Administration (FDA)|Spaulding Clinical Research LLC||May 2014||Phase 1|
|NCT02439658||Recruiting||Long QT Syndrome|Drug Toxicity||Massachusetts General Hospital|VA Office of Research and Development|Beth Israel Deaconess Medical Center|Brigham and Womens Hospital||January 2014||--|
|NCT01873950||Completed||Drug-induced Surface ECG Changes||Food and Drug Administration (FDA)|Spaulding Clinical Research LLC||May 2013||Phase 1|
|NCT00408200||Completed||Atrial Fibrillation||University of Pennsylvania||November 2006||--|
|NCT00392106||Suspended||Atrial Fibrillation||ProRhythm, Inc.||April 2006||Phase 3|
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